| Identification | Back Directory | [Name]
Atiratecan | [CAS]
867063-97-6 | [Synonyms]
TP300 Atiratecan CWJSAEZZZABNRI-HKBQPEDESA-N Glycine, glycyl-N-methyl-, (9S)-9-ethyl-9,10,13,15-tetrahydro-10,13-dioxo-1-pentyl-1H,12H-pyrano[3'',4'':6',7']indolizino[2',1':5,6]pyrido[4,3,2-de]quinazolin-9-yl ester | [Molecular Formula]
C31H34N6O6 | [MDL Number]
MFCD19443718 | [MOL File]
867063-97-6.mol | [Molecular Weight]
586.64 |
| Hazard Information | Back Directory | [Uses]
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. | [in vivo]
Atiratecan (TP300; 47 mg/kg; IV; once per week for 3 weeks) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP[1].
Atiratecan (24 mg/kg; IV; once per week for 6 weeks) in combination with capecitabine results in synergistic eVects in the HCT116 human colon cancer and NCI-N87 human gastric cancer xenograft models and an additive eVect in the WiDr human colon cancer xenograft model which is BCRP-positive and CPT-11-insensitive[1].
The eVective dose range of Atiratecan is between 0.30 and 47 mg/kg (MTD/ED50=157). The toxic dose is 63 mg/kg for Atiratecan[1].
| Animal Model: | Five-week-old male athymic nude mice (CAnN.CgFoxn1nu/CrlCrlj)[1] | | Dosage: | 47 mg/kg (the maximum tolerated dose; MTD) | | Administration: | IV; once per week for 3 weeks | | Result: | Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP.
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| [References]
[1] Endo M, et al. A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancerresistance protein-expressing tumor xenografts. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71. DOI:10.1007/s00280-009-1042-5 |
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